Eszopiclone

Oral
Insomnia

Debilitated patients and patients taking potent CYP3A4 inhibitors: Max: 2 mg at bedtime.

Severe: Max: 2 mg daily.

Should be taken on an empty stomach. Take immediately before going to bed. Avoid taking after a heavy meal.

Patient w/ history of drug dependence, resp compromise (e.g. COPD, sleep apnoea), depression, diseases or conditions that could affect metabolism or haemodynamic responses. Avoid abrupt withdrawal. Severe hepatic impairment. Elderly and debilitated patients. Pregnancy and lactation.

CNS depressant effects (e.g. impaired alertness and motor coordination), abnormal thinking, behavioural changes (e.g. hallucinations), amnesia and other neuropsychiatric symptoms, exacerbation of depression, suicidal thinking, complex behaviours (e.g. "sleep-driving"), unpleasant taste, headache, somnolence, resp infection, dizziness, dry mouth, dyspepsia, nausea, nervousness, rash, viral infection, anxiety, vomiting, confusion, decreased libido, dysmenorrhoea, gynecomastia, dysosmia.
Potentially Fatal: Anaphylaxis and angioedema.

PO: C

May impair ability to drive, operate machinery or other activities that require alertness. Take the medication when there is at least 7-8 hr of sleep.

Monitor patients w/ history of drug addiction, abuse, tolerance or dependence. Monitor patients for abnormal thinking or behaviour.

Symptoms: Impairment of consciousness ranging from somnolence to coma. Management: Symptomatic and supportive treatment w/ immediate gastric lavage. Administer IV fluids as needed. May give flumazenil.

Additive effects w/ CNS depressants (e.g. benzodiazepine, opioids, TCAs). Decreased exposure and effect w/ CYP3A4 inducers (e.g. rifampicin). Increased exposure and effect w/ CYP3A4 inhibitors (e.g. ketoconazole).

Onset of action may be reduced if taken w/ or immediately after a high-fat/heavy meal. Additive psychomotor impairment w/ alcohol.

Description:
Mechanism of Action: Eszopiclone may interact w/ γ-aminobutyric acid (GABA) receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Delayed w/ high-fat or heavy meal. Time to peak plasma concentration: Approx 1 hr.
Distribution: Plasma protein binding: 52-59%.
Metabolism: Extensively metabolised via oxidation and demethylation by CYP3A4 and CYP2E1 isoenzymes to several active and inactive metabolites.
Excretion: Via urine (up to 75%; as metabolites). Half-life: Approx 6 hr.

Source: National Center for Biotechnology Information. PubChem Database. Eszopiclone, CID=969472, https://pubchem.ncbi.nlm.nih.gov/compound/Eszopiclone (accessed on Jan. 22, 2020)

Store at 25°C.

Hypnotics & Sedatives

N05CF04 - eszopiclone ; Belongs to the class of benzodiazepine related drugs. Used as hypnotics and sedatives.

Anon. Eszopiclone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/11/2014.

Buckingham R (ed). Eszopiclone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/11/2014.

FDA warns of next-day impairment with sleep aid Lunesta (eszopiclone) and lowers recommended dose. U.S. FDA. https://www.fda.gov/. Accessed 25/08/2015.

Lunesta Tablet, Coated (Sunovion). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/11/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Eszopiclone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/11/2014.

Wickersham RM. Eszopiclone. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed 06/11/2014.